Modern chemotherapy can improve the quality of life of cancer patients via palliation of cancer-related symptoms, and can significantly extend survival in many malignancies as well. However, the inevitable toxic side-effects frequently limit dose intensity and frequency of drugs administration. For instance, the use of doxorubicin or cisplatin can effectively treat many malignancies, but the drug-induced cardiotoxicity and nephrotoxicity, respectively, limit their full potential. Thus, reducing undesired toxicity by selectively protecting normal cells without compromising cancer targeting would prove beneficial to chemotherapy and enhance clinical outcome.